Pda2 Test 3 Set 3

Front 1

Adrenocorticoid antagonists (2)

Back 1

1)metyrapone
2)trilostane

Front 2

Metyrapone mechanism

Back 2

inhibits 11beta hydroxylase (preventing cortisol synthesis)

Front 3

Trilostane mechanism

Back 3

inhibits 3beta deH AND 17alpha hydroxylase (preventing cortisol synthesis)

Front 4

...(2) are involved in spermatogenesis

Back 4

1)seminiferous tubules
2)sertoli cells (nutrition to sperm)

Front 5

Leydig or Interstitial cells fxn

Back 5

testosterone production

Front 6

Spermatogenesis/testosterone regulation (7)

Back 6

1)Hypothalamus releases GnRH
2)GnRH hits ant. pituitary and causes it to release FSH and LH
3)LH acts at leydig cells to release testosterone
4)FSH acts @ seminiferous tubule to release inhibin and increase spermatogenesis
5)Inhibin acts at hypothalamus and ant. pituitary to decr GnRH,FSH,LH
6)Testosterone acts at hypothalamus and ant. pituitary to decr GnRH,FSH,LH
7)Testosterone also acts at seminiferous tubules to incr Inhibin and incr spermatogenesis

Front 7

GnRH

Back 7

gonadotropin releasing hormone

Front 8

___ & ____ both MUST be present for spermatogeneis to occur

Back 8

1)FSH
2)testosterone

Front 9

Testosterone active metabolites and the enzymes required (2)

Back 9

1)dihydrotestosterone (5alpha reductase)
2)Estradiol (aromatase)

Front 10

Testosterone inactive metabolites and mechanism

Back 10

1)androsterone
2)etiocholanolone

liver metabolism

Front 11

Testosterone activity characteristics (2)

Back 11

1)high activity as itself in ant. pituitary and hypothalamus
2)low activity as itself in most tissues

Front 12

What is testosterone's most active metabolism?

Back 12

dihydrotestosterone, is active in most tissues

Front 13

2 groups of effects of testosterone

Back 13

1)androgenic effects (puberty sexual maturity)
2)anabolic effects (puberty growth)

Front 14

Androgenic effects of testosterone (7)

Back 14

1)growth of internal and external genital glands
2)vocal cords incr in length and thickness
3)beard and body hair grow
4)scalp hair thins and recedes
5)skin thickness increases
6)oily sebaceous gland secretion (acne)
7)CNS effects associated w/ sexual maturity

Front 15

Anabolic effects of testosterone (7)

Back 15

1)+ nitrogen balance
2)protein synthesis
3)incr muscle mass
4)weight gain
5)accelerated body growth
6)bone growth
7)closure of epiphysis (growth plate--is an estradiol effect)

Front 16

Absorption of Testosterone (2)

Back 16

a)Good thru GI but is rapidly first pass metabolized
b)esters are injected IM and absorbed slowly for ER

Front 17

How to incr activity of oral testosterone

Back 17

17alkalyation b/c liver metabolizes testosterone @ the 17-OH normally

Front 18

98% of testosterone is bound to...

Back 18

sex-hormone binding globulin and albumin

Front 19

Mechanism of testosterone in tissue (4)

Back 19

1)testosterone gets into cell and is converted to dihydrotestosterone via 5alpha reductase
2)it then binds an androgen receptor
3)then it binds to DNA and acts as a transcription factor
4)biologic activity follows

Front 20

Prototype of natural androgen

Back 20

Testosterone propionate (Testex)

Front 21

Prototype of orally active androgen

Back 21

Methyltestosterone (Virilron)

Front 22

Prototype of Transdermal Testosterone

Back 22

Testosterone Transdermal (Testoderm)

Front 23

Prototype of Anabolic steroid

Back 23

oxandrolone (oxandrin)

Front 24

How is a natural androgen defined?

Back 24

ratio of anabolic/androgenic activity is 1/1

Front 25

How is anabolic steroid defined?

Back 25

ratio of anabolic/androgenic activity is 2/1 to 15/1

Front 26

Primary uses of anabolic stimulation (2)

Back 26

1)used after major illness, burns, chemo to reverse the atrophy caused
2)illicit use in athletics

Front 27

Side effects of use of anabolic steroids (6)

Back 27

1)jaundice/liver cancer
2)edema
3)testicular atrophy
4)prostate hypertrophy leading to prostate cancer
5)feminizing effects in males
6)masculinization in females

Front 28

____ is observed in 80% of strength athletes due to anabolic steroids

Back 28

gynecomastia

Front 29

3 categories of antiandrogens

Back 29

1)synthesis inhibitors
2)5alpha reductase inhibitors
3)androgen receptor antagonists

Front 30

Androgen synthesis inhibitor drug

Back 30

GnRH (Leuprolide)

Front 31

GnRH (Leuprolide) mechanism and primary application

Back 31

inhibits LH secretion to decr testosterone production

prostate cancer

Front 32

5alpha reductase inhibitor mechanism and application

Back 32

reduces conversion of inactive testosterone to dihydrotestosterone

prostatic hypertrophy and male pattern baldness

Front 33

5alpha reductase inhibitor drug

Back 33

Finasteride (proscar)

Front 34

Androgen-Receptor Antagonists (2 and which is more potent)

Back 34

1)Spironolactone (Aldactone)
2)Flutamide (Eulexin)****

Front 35

Spironolactone mechanism and application

Back 35

1)weak androgen receptor antagonist and inhibits 17alpha hydroxylase
2)hirsutism in women

Front 36

Flutamide mechanism and application

Back 36

NON-steroidal receptor inhibitor that binds to androgen receptor and inhibits translocation to nucleus

Prostate cancer

Front 37

Flutamide works best if used w/...

Back 37

Leuprolide

Front 38

T/F
1. Testosterone is secreted from the Sertoli Cell
2. Testosterone is absorbed by the oral route of admin but is pharmacologically inactive
3. In most target tissues, testosterone must be metabolized to dihydrotestosterone in order to work

Back 38

1.False
2.True
3.True

Front 39

T/F
1. Testosterone is responsible for closure of the epiphysis in males
2. Flutamide is a steroid which inhibits 5alpha reductase

Back 39

1.True
2.False

Front 40

Biosynthesis steps for estradiol (1 enzyme) (5)

Back 40

1)Acetate to cholesterol
2)cholesterol to progesterone
3)Progesterone to Androstenedione
4)Androstenedione to testosterone
5)testosterone to estradiol via aromatase

Front 41

Secretory regulation of estradiol and progesterone (5)

Back 41

1)Puberty causes cerebral cortex to stimulate the hypothalamus the release GnRH
2)GnRH stimulates ant. pituitary to release FSH & LH
3)FSH & LH inhibits hypothalamus release of GnRH
4)FSH & LH stimulates ovary to release estradiol and progesterone
5)Estradiol and progesterone inhibit ant. pituitary release of FSH & LH, as well as hypothalamus release of GnRH

Front 42

FSH surge purpose in menses

Back 42

stimulates 4-6 follicles, 1 will mature

Front 43

LH surge purpose in menses

Back 43

ovulation

Front 44

Corpus luteum fxn (2)

Back 44

1)w/ LH stimulation it releases estrogen and progesterone
2)new menses cycle begins once it atrophies

Front 45

There are 2 surges of estrogen what are the causes?

Back 45

1)FSH effect on follicle
2)after ovulation LH stimulates the corpus luteum to release estrogen

Front 46

3 phases of endometrium

Back 46

1)FOLLICULAR PHASE- build up of endometrium b/c of estrogen stimualtion
2)LUTEAL PHASE- endometrium ready to be implanted b/c of estogen and progesterone
3)MENSES- endometrium sluffed off b/c no hormones to support it

Front 47

If pregnancy occurs what keeps estrogen/progesterone high? (2)

Back 47

1)Chorionic gonadotropin maintains CL to keep it releasing hormones
2)After 60 days, placenta produces the hormones

Front 48

What is the signal for labor and delivery?

Back 48

estrogen and progesterone fall off

Front 49

____ & ____ are needed to maintain the endometrium

Back 49

estrogen and progesterone

Front 50

Estrogen biological activity (3)

Back 50

1)changes that happen at puberty
2)secondary sexual characteristics
3)protective effect on bone and CV system

Front 51

SERM? (2)

Back 51

1)selective estrogen receptor modulators
2)act @ estrogen receptor to modulate estradiol activity

Front 52

Progesterone biological activity (4)

Back 52

1)axns are secondary to estrogen
2)needed for sexual development
3)menstrual regulation
4)pregnancy

Front 53

2 types of estrogen receptors (ER) and where they are found?

Back 53

1)ERalpha (reproductive tissue)
2)ERbeta (CV and bone)

Front 54

ER is a ____ receptor

Back 54

nuclear receptor

Front 55

Estrogen mechanism (3)

Back 55

1)estrogen binds to ER and a dimer is formed that recruits a coactivator
2)it is then able to bind DNA
3)acts as a transcription factor and elicits biological activity

Front 56

Estrogen mechanism is the same as _____

Back 56

progesterone's mechanism

Front 57

Estrogen ADM?

Back 57

A)readily absorbed
D)bound to sex hormone binding globulin and albumin
M)first pass metabolism in liver

Front 58

Difference in D b/w synthetic estrogen and endogenous

Back 58

synthetic are resistant to metabolism and are effective orally

Front 59

Natural estrogen prototype

Back 59

conjugated estrogens (premarin)

Front 60

Orally active estrogens prototype

Back 60

Ethinyl estradiol (estinyl)- used in OCs

Front 61

Synthetic estrogens prototype and 2 properties

Back 61

Diethylstillbesterol (stilphostrol)

nonsteroidal, orally active

Front 62

Transdermal estrogen prototype

Back 62

estradiol (estraderm)

Front 63

Adverse effects of estrogen (5)

Back 63

1)NAUSEA
2)fluid retention
3)CV (stroke, DVT)
4)breast cancer
5)chloasma (hyperpigmentation of skin/mask of pregnancy)

Front 64

Antiestrogens
a)other name
b)basic mechanism

Back 64

a)SERM
b)bind to ERalpha/beta and produce differing degrees of agonism/antagonism

Front 65

Natural progestins prototype
a)dosage forms(2)

Back 65

Progesterone acetate (Cyclin)
a)IM admin b/c poor GI absorption
b)gel for local intra-vaginal therapy

Front 66

Synthetic progestins prototype
a)dosage form
b)difference from natural

Back 66

Norethindrone (Norlutin)
a)oral activity
b)17 ethinyl to protect from 1st pass

Front 67

T/F
a)The PR is a membrane bound receptor
b)progesterone acts at the estrogen receptor
c)Estradiol reacts w/ a cytoplasmic receptor to increased intracellular cAMP

Back 67

a)false
b)false
c)false

Front 68

T/F
1)gonadotropins are secreted in a pulsitile manner
2)Estrogens have an aromatic A ring

Back 68

1)true
2)false?

Front 69

2 principle classes of female sex hormones

Back 69

1)estrogens
2)progestins

Front 70

Estrogens fxn (2)

Back 70

1)induce estrus
2)secondary sex characteristics

Front 71

Progestins fxn (2)

Back 71

1)reproduction
2)precursor to androgens, estrogens, adrenocorticoids

Front 72

Where are sex steroids produced in females (2)

Back 72

1)ovary
2)placenta

Front 73

Where are sex steroids produced in males

Back 73

testes

Front 74

Where are sex steroids produced in both males and females (3)

Back 74

1)adrenal cortex
2)hypothalamus
3)an. pituitary

Front 75

A ring in testosterone vs estrogen

Back 75

Both have an A ring but estrogen's is AROMATIC, testosterone's isnt

Front 76

Estradiol to testosterone?

Back 76

NOT possible, only the v.v. reaction

Front 77

17-20 lyase fxn

Back 77

converts 17alpha Hydroxypregnenolone to dehydroeplandrosterone via breaking off 2 carbons @ C17

Front 78

Cholesterol to pregnenolone via...

Back 78

break down of side chain of cholesterol

Front 79

Biosynthesis of sex steroids begins w/...

Back 79

cholesterol

Front 80

17alpha hydroxylase fxn

Back 80

pregnenolone to progesterone

Front 81

_____ leads to male and female sex hormones (estradiol and testosterone)

Back 81

Androstenedione****

Front 82

Fxn of aromatase

Back 82

aromatizes A ring of androstenedione

Front 83

3 estrogens in the body

Back 83

1)estradiol
2)estrone
3)estriol

Front 84

Estradiol to estrone and v.v. via....

Back 84

estradiol deH

Front 85

Estrogen metabolism mainly occurs @...by...

Back 85

A ring by adding OH onto the A ring via estrogen2/4 hydroxylase, making it metabolizable by COMT

Front 86

Inactive metabolites of estrogen and how you get them

Back 86

2/4 methoxy estrogens that are inactivated by COMT

Front 87

Estrogens are eliminated from the body via...(3)

Back 87

1)Glucuronide
2)sulfate
3)glutathione conjugates
thru the urine and this must all occur @ a free OH

Front 88

Most potent endogenous androgen

Back 88

5alpha dihydrotestosterone

Front 89

Androgen metabolism occurs where? (and what is the major site) (4)

Back 89

1)LIVER***
2)prostate gland
3)ovarian tissue
4)adipose tissue

Front 90

How are androgens excreted in the urine (2)

Back 90

via glucuronide and sulfate conjugations

Front 91

Inactivation of androgens occurs when...

Back 91

alpha/beta H @ C5 and keto group goes to alphaOH

Front 92

____ was found in excess in Floyd Landis

Back 92

androsterone

Front 93

Structural features of estrogens (5)

Back 93

1)aromatic A ring
2)phenolic OH @ C3
3)17beta OH
4)distance b/w 2 OH's is 8.55 angstroms
5)planar hydrophobic molecule

Front 94

Which is more active and why? estrone vs. estradiol

Back 94

estradiol b/c it has the 17beta OH and estrone does NOT

Front 95

What can be done to estrogens to reduce their activity? (5)

Back 95

1)insert OH @ C6,7,11
2)remove oxygen fxn from C3,17
3)epimerization of 17beta OH to alpha
4)unsaturation into B ring
5)enlargement of D ring

Front 96

What can be done to increase estrogen activity

Back 96

NOTHING

Front 97

AAs @ the estrogen receptor AS that interact w/ estradiol (3)

Back 97

1)histidine
2)glutamate
3)arginine

Front 98

Female sex hormone derivatives are ____.... (3)

Back 98

Estradiol derivatives
1)usually esterified to make orally active and incr half-life
2)or put on ethinyl @ C17
3)put ether on A ring